| Identification | Back Directory | [Name]
(R)-(1-(4-fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-1,4,5,6,7,8-hexahydro-4aH-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone | [CAS]
1496510-51-0 | [Synonyms]
EOS-61931
CORT-125134
[(4aR)-1-(4-fluorophenyl)-6-(1-methylpyrazol-4-yl)sulfonyl-4,5,7,8-tetrahydropyrazolo[3,4-g]isoquinolin-4a-yl]-[4-(trifluoromethyl)pyridin-2-yl]methanone
(R)-(1-(4-fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-1,4,5,6,7,8-hexahydro-4aH-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone
Methanone, [(4aR)-1-(4-fluorophenyl)-1,4,5,6,7,8-hexahydro-6-[(1-methyl-1H-pyrazol-4-yl)sulfonyl]-4aH-pyrazolo[3,4-g]isoquinolin-4a-yl][4-(trifluoromethyl)-2-pyridinyl]- | [Molecular Formula]
C27H22F4N6O3S | [MDL Number]
MFCD33029252 | [MOL File]
1496510-51-0.mol | [Molecular Weight]
586.56 |
| Chemical Properties | Back Directory | [Boiling point ]
715.8±70.0 °C(Predicted) | [density ]
1.54±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
0.24±0.40(Predicted) | [color ]
White to off-white | [InChIKey]
WANIDIGFXJFFEL-SANMLTNESA-N | [SMILES]
C([C@@]12C(=CC3N(C4=CC=C(F)C=C4)N=CC=3C1)CCN(S(C1=CN(C)N=C1)(=O)=O)C2)(C1=NC=CC(C(F)(F)F)=C1)=O |
| Hazard Information | Back Directory | [Uses]
Relacorilant is a potent, selective and orally bioavailable glucocorticoid receptor antagonist, with a Ki of 7.2 nM in HepG2 TAT assay, and also shows Kis of 12, 81.2, 210 nM for rat, human and monkey glucocorticoid receptor in cell-based assay, respectively. Relacorilant has the potential for Cushing’s syndrome treatment. | [in vivo]
Relacorilant (30 mg/kg, p.o., twice a day) dramaticlly blocks the effects on plasma insulin and completely inhibits cortisone induced increase in plasma glucose in rats of exogenous Cushing’s syndrome, and similar effect is also observed when administrated with of Relacorilant at 7.5 mg/kg twice a day[1]. | [References]
[1] Hunt HJ, et al. Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist. J Med Chem. 2017 Apr 27;60(8):3405-3421. DOI:10.1021/acs.jmedchem.7b00162 |
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